Name: Dapoxetine HCl
Brand: Selleck Chemicals
SKU: S1869
Rating: 5 (1 reviews)

Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.

Dapoxetine HCl Chemical Structure

CAS: 129938-20-1

Purity & Quality Control

Batch: Purity: 99.98%

99.98

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Signaling Pathway

5-HT Receptor Signaling Pathway

Choose Selective 5-HT Receptor Inhibitors

Biological Activity

Description

Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.

Targets

5-HT ^[1]

In vitro
In vitro	Dapoxetine not only reduces the peak amplitude of Kv4.3 currents but also accelerates the decay rate of current inactivation in a concentration-dependent manner. Dapoxetine decreases the integral of the Kv4.3 currents over the duration of a depolarizing pulse with an IC50 of 5.3 μM. Dapoxetine also causes a substantial acceleration in closed-state inactivation. Dapoxetine produces a significant use-dependent block, which is accompanied by a delayed recovery from inactivation of Kv4.3 currents. ^[1] Dapoxetine decreases the peak amplitude of Kv1.5 currents and accelerates the decay rate of current inactivation in a concentration-dependent manner with an IC50 of 11.6 μM. Dapoxetine decreases the tail current amplitude and slows the deactivation process of Kv1.5, which results in a tail crossover phenomenon. Dapoxetine produces a use-dependent block of Kv1.5 at frequencies of 1 and 2 Hz and slowed the time course for recovery of inactivation. ^[2] Dapoxetine also appears to be a useful adjunct to morphine, lowering the threshold for analgesia, although Dapoxetine itself has negligible analgesic activity. Dapoxetine is the D-enantiomer of LY 243917 and is 3.5 times more potent as a serotonin reuptake inhibitor than the L-enantiomer. ^[3]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT03018743	Unknown status	Premature Ejaculation	Pusan National University Hospital	January 2017	--
NCT01928563	Unknown status	Healthy Male Subjects	Dong-A Pharmaceutical Co. Ltd.\|Dong-A ST Co. Ltd.	September 2013	Phase 1
NCT01366664	Completed	Ejaculation	Janssen Research & Development LLC	April 2011	Phase 1
NCT01063881	Completed	Sexual Dysfunction Physiological	Johnson & Johnson Pte Ltd	May 2010	Phase 3
NCT00211094	Completed	Ejaculation	Alza Corporation DE USA		Phase 3

References

Chemical Information & Solubility

Molecular Weight	341.87	Formula	C₂₁H₂₃NO.HCl
CAS No.	129938-20-1	SDF	Download Dapoxetine HCl SDF
Smiles	CN(C)C(CCOC1=CC=CC2=CC=CC=C21)C3=CC=CC=C3.Cl
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 68 mg/mL ( (198.9 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 68 mg/mL

Ethanol : 68 mg/mL

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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Handling Instructions

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